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ChEMBL ligand: CHEMBL1800807 (Anacetrapib, MK-0859, MK0859) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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cholesteryl ester transfer protein/Cholesteryl ester transfer protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3572] [GtoPdb: 3248] [UniProtKB: P11597] | ||||||||
ChEMBL | Inhibition of full-length human recombinant CETP expressed in CHO cells by BODIPY-CE dye based fluorescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2016) 24: 1811-1818 [PMID:26993745] |
ChEMBL | Inhibition of CETP in 95% human serum assessed as inhibition of transfer of [3H] cholesteryl oleate or [3H] triolein between LDL and HDL | B | 7.28 | pIC50 | 53 | nM | IC50 | Bioorg Med Chem Lett (2021) 32: 127668-127668 [PMID:33161125] |
ChEMBL | Inhibition of CETP in human plasma assessed as reduction in fluorescent intensity by fluorescence analysis | B | 7.34 | pIC50 | 46 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3056-3062 [PMID:22497761] |
ChEMBL | Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein between exogenous [3H]LDL in 95% human serum by liquid scintillation analysis | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2021) 64: 13215-13258 [PMID:34375108] |
ChEMBL | Inhibition of recombinant CETP (unknown origin) assessed as inhibition of BODIPY-labeled cholesteryl transfer to fluorescent substrate by fluorimetric assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2016) 123: 419-430 [PMID:27490022] |
ChEMBL | Inhibition of recombinant full length human CETP expressed in CHO cells assessed as reduction in BODIPY-CE transfer measured after 1 to 3 hrs by fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2017) 126: 143-153 [PMID:27750148] |
ChEMBL | Inhibition of human CETP | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 126824-126824 [PMID:31780304] |
ChEMBL | Inhibition of recombinant human CETP after 3 hrs using fluorescent cholesteryl containing HDL after 3 hrs by fluorescence assay | B | 7.47 | pIC50 | 33.8 | nM | IC50 | Eur J Med Chem (2017) 139: 201-213 [PMID:28802120] |
ChEMBL | Inhibition of CETP in human plasma measured every 30 mins for 120 mins by fluorescence method | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2017) 60: 8466-8481 [PMID:29035537] |
GtoPdb | - | - | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2011) 54: 4880-95 [PMID:21682257] |
ChEMBL | Inhibition of human recombinant CETP-mediated cholesteryl ester transfer activity after 1 hr by fluorescent cholesteryl esters transfer assay | B | 7.76 | pIC50 | 17.2 | nM | IC50 | J Med Chem (2011) 54: 4880-4895 [PMID:21682257] |
ChEMBL | Inhibition of CETP-mediated neutral lipid transfer by fluorometric analysis | B | 7.76 | pIC50 | 17.2 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 199-203 [PMID:22142541] |
ChEMBL | Inhibition of recombinant CETP (unknown origin) assessed as inhibition of transfer of [3H]cholesteryl oleate or [3H]triolein using exogenous LDL and HDL in 2% human serum by liquid scintillation analysis | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2021) 64: 13215-13258 [PMID:34375108] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of [S35]-MK-0499 binding to human ERG expressed in HEK293 cells | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2021) 64: 13215-13258 [PMID:34375108] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]